31 results about "Aprepitant" patented technology

Disclosed herein include methods, compositions, and kits suitable for use in preventing or relieving side effects associated with the administration of a weight loss medication. The method can comprise administering to a subject under a weight loss treatment a composition comprising a neurokinin 1 receptor (NK1R) antagonist (e.g., aprepitant).

The invention discloses an aprepitant nano suspension pharmaceutical composition and a preparation method thereof. The aprepitant nano suspension pharmaceutical composition comprises aprepitant, a space stabilizer, an electrostatic stabilizer and water, the steric stabilizer is selected from one or more of poloxamer F188, poloxamer F407 and polyvinylpyrrolidone K30, and the steric stabilizer is selected from one or more of poloxamer F188, poloxamer F407 and polyvinylpyrrolidone K30; the electrostatic stabilizer is lauryl sodium sulfate or PCM. By selecting a specific stabilizer and a preparation method, subcutaneous injection of aprepitant is realized, the stability of the medicine is remarkably improved, and the medicine loading capacity is increased. In addition, according to the method, the preparation process is simplified, the formula screening time is shortened, and therefore the overall preparation time is shortened.

The invention belongs to the technical field of medicine, and particularly relates to an aprepitant nanocrystalline composition and a preparation method and application thereof.The aprepitant and a sucrose solution are mixed, a stabilizer is added to obtain a solution to be ground, the solution to be ground is ground through a wet grinding process, and the aprepitant nanocrystalline composition is obtained; uniformly mixing the suspension with a spray drying protective agent and a flow aid to obtain a mixed solution, and drying and curing the mixed solution by adopting a spray dryer to obtain the aprepitant nanocrystal composition in the form of a dry suspension, and directly spray-drying the suspension, uniformly mixing the suspension with a skeleton agent and an adhesive, adding water to a constant volume, carrying out vacuum degassing, and carrying out pre-freezing and freeze-drying to obtain the freeze-dried orally disintegrating tablet type aprepitant nanocrystal composition.

Disclosed herein are pharmaceutical compositions in the form of a suspension for oral delivery. Some embodiments provide a pharmaceutical composition in the form of a suspension for oral delivery comprising an active pharmaceutical ingredient; water, a suspending agent; a buffering agent; and one or more of a wetting agent and a binder / filler. In some embodiments, the active pharmaceutical ingredient is selected from quetiapine, sildenafil, tadalafil, cinacalcet, ticagrelor, mycophenolate, aprepitant, zonisamide, and primidone.

Disclosed are a pharmaceutical composition, an aprepitant injection, and an aprepitant freeze-dried powder injection. The pharmaceutical composition comprises aprepitant, a primary stabilizer, and a secondary stabilizer, wherein the primary stabilizer comprises sodium deoxycholate and the secondary stabilizer comprises povidone. The aprepitant injection can be administered by injecting. The formulation uses a largely reduced amount of excipients, and is less irritative to an injection site, less prone to cause a hypersensitive reaction, and thus safer when being used by a patient. The formulation has good stability and can be stored and transported at room temperature, largely reducing production, storage, and transportation costs.

The present invention belongs to the field of biopharmaceuticals, and specifically relates to a high-dissolution aprepitant formulation and a preparation method thereof. The high-dissolution aprepitant formulation comprises the following components in parts by weight: 50-80 parts of aprepitant, 5-10 parts of a surfactant, 20-40 parts of a filler, 5-10 parts of a disintegrant, and 0.5-3 parts of a lubricant; wherein the surfactant is composed of triethanolamine oleate and another surfactant, and the other surfactant is selected from one or more of Span 20, Span 40, Span 60, Span 80, and Span 83. The present invention has found that by using a combination of triethanolamine oleate and the other surfactant, the solubility of aprepitant can be effectively improved and its dissolution can be promoted. At the same time, the preparation process is simple and does not bring excessive cost pressure to the process.

Disclosed are a pharmaceutical composition, an aprepitant injection, and an aprepitant freeze-dried powder injection. The pharmaceutical composition comprises aprepitant, a primary stabilizer, and a secondary stabilizer, wherein the primary stabilizer comprises sodium deoxycholate and the secondary stabilizer comprises povidone. The aprepitant injection can be administered by injecting. The formulation uses a largely reduced amount of excipients, and is less irritative to an injection site, less prone to cause a hypersensitive reaction, and thus safer when being used by a patient. The formulation has good stability and can be stored and transported at room temperature, largely reducing production, storage, and transportation costs.

The invention belongs to the field of medicine, and provides an aprepitant micelle composition and a preparation method thereof, the aprepitant micelle composition is composed of an active component aprepitant and auxiliary materials such as phospholipid, cholic acid or a salt thereof, a nano-micelle stabilizer, a pH regulator and the like, the dosage form is a freeze-dried powder injection, and the solubility of the aprepitant is remarkably improved; the combination of the nano-micelle stabilizer can significantly improve the stability of the preparation, avoids the use of a large amount of soybean oil for solubilization, and reduces the risk of hyperlipidemia. Ethanol is not contained, so that ethanol anaphylaxis is avoided, and the safety of clinical medication can be remarkably improved. After the freeze-dried powder injection is redissolved, a hot-pressing sterilization mode can be adopted, so that the sterile guarantee level is remarkably improved, and the clinical medication risk is reduced. The aprepitant micelle composition is prepared by adopting a tert-butyl alcohol-water freeze-drying method, the process is simple and convenient, large-scale production is easy, a common freeze-dried powder injection production line can be adopted, special equipment such as a high-pressure homogenizer and a special fat emulsion production line are not needed, and the production cost can be remarkably reduced.

The present disclosure relates to an injectable pharmaceutical composition comprising a plurality of liposomes each comprising aprepitant, a phospholipid and a surfactant; a tonicity agent; and water, as well as to a method of manufacturing said injectable pharmaceutical composition, and a container comprising said pharmaceutical composition.

Amorphous solid dispersions significantly improve the solubility problems associated with Aprepitant. Finished dosage forms as well as processes for their preparation are provided.

The invention belongs to the technical field of pharmaceutical preparations, and discloses a stable aprepitant injection and a preparation method thereof. The aprepitant injection comprises the following raw materials in percentage by mass: 0.5-1% of aprepitant, 8-12% of soybean oil, 8-12% of egg yolk lecithin, 0.05-2% of egg yolk phosphatidyl glycerol, 0.5-0.8% of sodium oleate, 5-8% of cane sugar, 2-4% of ethanol and the balance of water for injection, totaling 100%. The selected co-emulsifier egg yolk phosphatidyl glycerol has two hydroxyl groups at the hydrophilic end, so that the egg yolk phosphatidyl glycerol has extremely strong emulsifying performance, is well compatible with aprepitant, has a good emulsifying effect of the preparation, and can well encapsulate aprepitant, so that the dosage of egg yolk lecithin is reduced by about one third, and the stable drug-loaded fat emulsion is formed; the preparation method is suitable for industrial production, the preparation cost is low, and the accessibility of the medicine is improved.

The present disclosure provides pharmaceutical formulations including aprepitant that are suitable for intravenous administration, including lyophilized formulations, processes for the preparation thereof, and their use in the treatment or prevention of emesis.

The invention relates to the field of medicinal chemistry, in particular to a small-molecule coupling medicine as well as a preparation method and application thereof. The structural formula of the micromolecular coupling drug is shown as a formula 1: # imgabs0, wherein A in the formula 1 is a cytotoxic drug. According to the small-molecule coupled drug provided by the invention, two parts of structures are connected to a cytotoxic drug, one part is a tetrafluoro azidophenyl connexon which can be activated by X-rays to release the cytotoxic drug, and the other part is a small-molecule inhibitor aprepitant with targeting NK1R, so that drug targeting can be better realized; meanwhile, medicine activation can be realized in a time-space controllable manner, the compound can be well applied to tumor treatment, and the compound shows higher cytotoxicity to tumor cells after being irradiated by X rays.

1. Name of the design product: packaging box (Aprepitant capsule). 2. Use of the design product: the design product is used for the packaging of medicines. 3. Design points of the design product: the combination of shape and pattern. 4. Picture or photo best indicating the design points: perspective view.

The present invention relates to an emulsion including aprepitant, an emulsifier, an oil, polyethylene glycol, and water, without substantial addition of ethanol.

The application discloses a pharmaceutical composition, an aprepitant injection and an aprepitant freeze-dried powder injection. The pharmaceutical composition comprises aprepitant, a primary stabilizer and a secondary stabilizer, wherein the primary stabilizer comprises sodium deoxycholate, and the secondary stabilizer comprises povidone. The aprepitant injection provided by the application can be injected for administration, the dosage of auxiliary materials is greatly reduced, the injection site is less irritating when used by patients, and the aprepitant injection is less likely to cause hypersensitivity reaction and is safer; the preparation has good stability, can be stored and transported at room temperature, and greatly reduces the production, storage and transportation costs.

Disclosed herein include methods, compositions, and kits suitable for use in preventing and treating Alzheimer's disease. In some embodiments, methods of delaying or reducing the likelihood of onset of Alzheimer's disease are provided. The method can comprise administering to a subject in need thereof a composition comprising a neurokinin 1 receptor (NK1R) antagonist (e.g., aprepitant).

Disclosed herein are pharmaceutical compositions in the form of a suspension for oral delivery. Some embodiments provide a pharmaceutical composition in the form of a suspension for oral delivery comprising an active pharmaceutical ingredient; water; a suspending agent; a buffering agent; and one or more of a wetting agent and a binder / filler. In some embodiments, the active pharmaceutical ingredient is selected from quetiapine, sildenafil, tadalafil, cinacalcet, ticagrelor, mycophenolate, aprepitant, zonisamide, and primidone.

The utility model discloses a closed reaction kettle for producing aprepitant. The closed reaction kettle comprises a kettle body, the feeding hole is formed in the kettle body; the discharge hole is formed in the kettle body; the base is arranged on the kettle body; the mounting block is arranged on the base opposite to the other side of the kettle body; the speed reducer is arranged on the mounting block opposite to the other side of the base; the motor is arranged on the speed reducer opposite to the other side of the mounting block; and the stirring mechanism is connected with the speed reducer and the kettle body. According to the closed reaction kettle for aprepitant production disclosed by the utility model, the stirring block can be replaced, the operation is simple, and the storage of more other stirring parts is avoided.

The present invention relates to an injectable composition comprising aprepitant and at least one pharmaceutically acceptable excipient. The invention further relates to processes for preparing such injectable compositions and to their use in the prevention or treatment of emesis, including but not limited to chemotherapy- induced or postoperative nausea and vomiting.

The invention belongs to the field of biological medicine, and particularly relates to a high-dissolution aprepitant preparation and a preparation method thereof. The high-dissolution aprepitant preparation is prepared from the following components in parts by weight: 50 to 80 parts of aprepitant, 5 to 10 parts of a surfactant, 20 to 40 parts of a filling agent, 5 to 10 parts of a disintegrating agent and 0.5 to 3 parts of a lubricating agent, wherein the surface active agent is composed of triethanolamine oleate and another surface active agent, and the other surface active agent is selected from one or more of span 20, span 40, span 60, span 80 and span 83. It has been found that by adopting the combination of triethanolamine oleate and another surfactant, the solubility of aprepitant can be effectively improved, dissolution of aprepitant is promoted, meanwhile, the preparation technology is simple, and too high cost pressure cannot be brought to the technological process.

The present invention belongs to the field of medicine and provides an aprepitant micelle injection and a preparation method thereof. The aprepitant micelle injection is composed of an active ingredient aprepitant, a phospholipid, bile acid or a salt thereof, a nano-micelle stabilizer, a pH regulator and water for injection. The above scheme selects a phospholipid and bile acid micelle system with good physiological compatibility and good safety for solubilization, thereby significantly improving the solubility of aprepitant; the combined use of the nano-micelle stabilizer can significantly improve the stability of the preparation; avoids the use of a large amount of soybean oil for solubilization, thereby reducing the risk of lipid metabolism; does not contain ethanol to avoid ethanol allergic reactions, thereby improving the safety of clinical medication; adopts a hot press sterilization method, thereby improving the sterility assurance level; the process is simple, easy to scale up for production, similar to the production process of ordinary injections, does not require special equipment such as a high-pressure homogenizer and a dedicated fat emulsion production line, and can significantly reduce production costs.

Disclosed herein include methods, compositions, and kits suitable for use in preventing, slowing the progression of or treating obesity and weight controlling. The method can comprise administering to a subject a composition comprising a neurokinin 1 receptor (NK1R) antagonist (e.g., aprepitant) and a cyclic dipeptide (e.g., cyclo(His-Pro)).

Disclosed herein include methods, compositions, and kits suitable for use in treating and preventing hair loss. The composition includes a neurokinin 1 receptor (NK1R) antagonist (e.g., aprepitant or a pharmaceutically acceptable salt, solvate, stereoisomer, prodrug thereof). The composition can be formulated in form of ointment, gel, lotion, cream, paste, powder, pill, tablet, microtablet, pellet, micropellet, capsule, capsule containing microtablets, solution, suspension, emulsion, aerosols, or nanoparticles. The method of treating or preventing hair loss, comprises administering to a subject a therapeutically or prophylactically effective amount of a composition herein described, for example, by topical application.

The present disclosure provides a compound emulsion for injection of aprepitant and palonosetron hydrochloride. The compound emulsion has good stability and is more convenient and effective in preventing and treating nausea and vomiting, which improves patient medication adherence.

Disclosed herein are novel pharmaceutical formulations of aprepitant suitable for parenteral administration including intravenous administration. Also included are formulations including both aprepitant and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy.

Disclosed herein are pharmaceutical compositions in the form of a suspension for oral delivery. Some embodiments provide a pharmaceutical composition in the form of a suspension for oral delivery comprising an active pharmaceutical ingredient; water; a suspending agent; a buffering agent; and one or more of a wetting agent and a binder / filler. In some embodiments, the active pharmaceutical ingredient is selected from quetiapine, sildenafil, tadalafil, cinacalcet, ticagrelor, mycophenolate, aprepitant, zonisamide, and primidone.